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Mixed-Charged Zwitterionic Polymeric Micelles for Tumor Acidic Environment Responsive Intracellular Drug Delivery.
Langmuir ( IF 3.7 ) Pub Date : 2018-07-10 , DOI: 10.1021/acs.langmuir.8b00471 Zhihui Qin 1 , Tingting Chen 1 , Wenzhuo Teng 1 , Qiao Jin 1 , Jian Ji 1
Langmuir ( IF 3.7 ) Pub Date : 2018-07-10 , DOI: 10.1021/acs.langmuir.8b00471 Zhihui Qin 1 , Tingting Chen 1 , Wenzhuo Teng 1 , Qiao Jin 1 , Jian Ji 1
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A new class of mixed-charged zwitterionic copolymer poly(aminoethyl methacrylate)- co-poly(methacrylic acid)- co-poly( n-butyl methacrylate) (CPMA) was prepared as drug nanocarrier for efficient intracellular delivery of Doxorubicin (DOX). The mixed-charged CPMA copolymer could readily assemble to micelles in physiological environment (pH 7.4) with the size of 42.6 nm and zeta potential of -26 mV, which would lead to a prolonged circulation time and enhanced tumor penetration. However, the micelles formed large aggregates due to the protonation of carboxyl groups at extracellular tumor pH (pH 6.5). Meanwhile, the zeta potential of CPMA micelles increased from -26 mV to -6 mV when the solution pH was changed from pH 7.4 to pH 6.5. The increase of size and zeta potential at extracellular tumor pH could benefit the retention of micelles in tumor matrix and uptake by cancer cells. The DOX-loaded mixed-charged CPMA micelles could induce a higher internalization at pH 6.5 than 7.4 at varied time periods. Moreover, cytotoxicity assay demonstrated that the blank micelles showed excellent biocompatibility, but were highly cytotoxic toward KB cells after loading with DOX. Thus, the mixed-charged zwitterionic polymeric micelles might be a promising carrier for tumor acidic environment responsive drug delivery.
中文翻译：
用于肿瘤酸性环境响应性细胞内药物传递的混合充电两性离子聚合物胶束。
制备了一类新型的带电荷的两性离子共聚物聚甲基丙烯酸氨基乙酯-共聚甲基丙烯酸共聚甲基丙烯酸正丁酯（CPMA）作为药物纳米载体，以有效地递送阿霉素（DOX）。混合电荷的CPMA共聚物可以在生理环境（pH 7.4）中容易地组装成胶束，尺寸为42.6 nm，ζ电位为-26 mV，这将导致延长的循环时间和增强的肿瘤渗透性。然而，由于细胞外肿瘤pH（pH 6.5）下羧基的质子化，这些胶束形成了大的聚集体。同时，当溶液的pH从pH 7.4改变为pH 6.5时，CPMA胶束的ζ电势从-26 mV增加到-6 mV。在细胞外肿瘤pH下大小和ζ电势的增加可有利于胶束在肿瘤基质中的保留和癌细胞的摄取。负载DOX的混合电荷CPMA胶束在不同时间段可诱导pH 6.5高于7.4的内在化。此外，细胞毒性试验表明空白胶束具有优异的生物相容性，但在装载DOX后对KB细胞具有高度的细胞毒性。因此，混合电荷的两性离子聚合物胶束可能是肿瘤酸性环境响应性药物递送的有前途的载体。但在装载DOX后，对KB细胞具有高度的细胞毒性。因此，混合电荷的两性离子聚合物胶束可能是肿瘤酸性环境响应性药物递送的有前途的载体。但在装载DOX后，对KB细胞具有高度的细胞毒性。因此，混合电荷的两性离子聚合物胶束可能是肿瘤酸性环境响应性药物递送的有前途的载体。
更新日期：2018-06-25
中文翻译：
用于肿瘤酸性环境响应性细胞内药物传递的混合充电两性离子聚合物胶束。
制备了一类新型的带电荷的两性离子共聚物聚甲基丙烯酸氨基乙酯-共聚甲基丙烯酸共聚甲基丙烯酸正丁酯（CPMA）作为药物纳米载体，以有效地递送阿霉素（DOX）。混合电荷的CPMA共聚物可以在生理环境（pH 7.4）中容易地组装成胶束，尺寸为42.6 nm，ζ电位为-26 mV，这将导致延长的循环时间和增强的肿瘤渗透性。然而，由于细胞外肿瘤pH（pH 6.5）下羧基的质子化，这些胶束形成了大的聚集体。同时，当溶液的pH从pH 7.4改变为pH 6.5时，CPMA胶束的ζ电势从-26 mV增加到-6 mV。在细胞外肿瘤pH下大小和ζ电势的增加可有利于胶束在肿瘤基质中的保留和癌细胞的摄取。负载DOX的混合电荷CPMA胶束在不同时间段可诱导pH 6.5高于7.4的内在化。此外，细胞毒性试验表明空白胶束具有优异的生物相容性，但在装载DOX后对KB细胞具有高度的细胞毒性。因此，混合电荷的两性离子聚合物胶束可能是肿瘤酸性环境响应性药物递送的有前途的载体。但在装载DOX后，对KB细胞具有高度的细胞毒性。因此，混合电荷的两性离子聚合物胶束可能是肿瘤酸性环境响应性药物递送的有前途的载体。但在装载DOX后，对KB细胞具有高度的细胞毒性。因此，混合电荷的两性离子聚合物胶束可能是肿瘤酸性环境响应性药物递送的有前途的载体。
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